Methacholine bromide
(Synonyms: Acetyl-β-methylcholine bromide) 目录号 : GC67620
Methacholine (Acetyl-β-methylcholine) bromide 是一种有效的 muscarinic-3 (M3) 激动剂。Methacholine bromide 直接作用于平滑肌上的乙酰胆碱受体，导致支气管收缩和气道变窄。Methacholine bromide 对识别支气管高反应性 (BHR) 显示出高灵敏度。Methacholine bromide 可用于测量气道高反应性 (AHR)，作为评估具有哮喘样症状和正常静息呼气流速的个体的诊断辅助[2]。
Cas No.:333-31-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Methacholine (Acetyl-β-methylcholine) bromide is a potent muscarinic-3 (M3) agonist. Methacholine bromide acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine bromide shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine bromide can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates[1][2][3][4].
Methacholine bromide (0.5 µg/kg plus 5 µg/kg/min for 30 min) induces bronchoconstriction in dogs[4].
Methacholine bromide (0.5 mg/kg; i.v.) induces bronchoconstriction was inhibited by bradykinin (4-40 µg/kg; i.v.) in a a dose-dependent manner in mouse[5].
| Animal Model: | 9-week female BALB/c mice[6] |
| Dosage: | 0.03, 0.1, 0.3, 1 mg/kg |
| Administration: | I.v |
| Result: | Induced severe bronchoconstriction. |
[1]. Cohen J, et al. Relationship between airway responsiveness to neurokinin A and methacholine in asthma. Pulm Pharmacol Ther. 2005;18(3):171-176.
[2]. Anderson SD, et al. Comparison of mannitol and methacholine to predict exercise-induced bronchoconstriction and a clinical diagnosis of asthma. Respir Res. 2009;10(1):4. Published 2009 Jan 23.
[3]. Cockcroft DW. Methacholine challenge methods. Chest. 2008;134(4):678-680.
[4]. Kabara S, et al. Differential effects of thiopental on methacholine- and serotonin-induced bronchoconstriction in dogs. Br J Anaesth. 2003 Sep;91(3):379-84.
[5]. Folkerts G, et al. Bradykinin causes inhibition of methacholine-induced bronchoconstriction in vivo in mice. Naunyn Schmiedebergs Arch Pharmacol. 2001 Jul;364(1):53-8.
[6]. Vitorasso RL, et al. Methacholine dose response curve and acceptability criteria of respiratory mechanics modeling. Exp Lung Res. 2020 Feb-Mar;46(1-2):23-31.
| Cas No. | 333-31-3 | SDF | Download SDF |
| 别名 | Acetyl-β-methylcholine bromide | ||
| 分子式 | C8H18BrNO2 | 分子量 | 240.14 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1642 mL | 20.8212 mL | 41.6424 mL |
| 5 mM | 0.8328 mL | 4.1642 mL | 8.3285 mL |
| 10 mM | 0.4164 mL | 2.0821 mL | 4.1642 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Ipratropium bromide in the recovery phase after Methacholine PD20: is there more than an antagonist effect?
Allergol Immunopathol (Madr) 1998 Nov-Dec;26(6):273-6.PMID:9934405doi
Aim of the study was to discover whether the recovery phase after Methacholine challenge might be influenced by the administration of an antimuscarinic drug and to verify the mode and timescale of restored receptor activity. 16 patients with severe bronchial hyperreactivity were selected and subjected to Methacholine test in order to assess: the preventive bronchodilatory effect of ipratropium bromide (40 mcg) inhaled before the test and the bronchial spasm spontaneous recovery after PD20 at 15, 30 and 60 minutes. Data were subjected to variance and Tukey test analysis. The results confirm that ipratropium bromide raises the Methacholine dose response threshold by a factor of about 10 and also demonstrate that the anti-muscarinic drug modified the FEV1 PD20 and influenced the recovery phase by intensifying and making the bronchial spasm resolution faster. Thus results moreover suggest that the receptor activity restoration depends also on the elimination of the muscarinic mediator.
Ipratropium bromide: bronchodilator action and effect on methacholine-induced bronchoconstriction
J Asthma 1987;24(1):29-35.PMID:2975285DOI:10.3109/02770908709073190.
The effects of ipratropium bromide (80 and 200 micrograms) and placebo on the basal bronchial tone and on methacholine-induced bronchoconstriction were investigated in 10 asthmatic patients in a placebo-controlled double-blind manner. Bronchial hyperreactivity to Methacholine was confirmed at a pretrial bronchial challenge. The patients were randomly allocated to two groups in which the drug was inhaled from either metered-dose inhalers (MDI) or powder capsules. With the high dosage, the bronchodilation resulting from powder capsules was somewhat more pronounced than that achieved with the MDI. Otherwise the bronchodilator effect of ipratropium bromide and the protection afforded by the drug against methacholine-induced bronchoconstriction were similar in the two groups. In five patients the bronchodilator effect was better and in four patients the tolerance to Methacholine was greater after the higher ipratropium dosage than after the lower one. In two patients ipratropium bromide had no bronchodilator effect but gave good protection against methacholine-induced bronchoconstriction. It is concluded that some patients benefit from a dosage of ipratropium bromide higher than that usually recommended and that an anticholinergic effect on the bronchi is possible even in the absence of the bronchodilator effect in the basal state.
Ipratropium bromide (Atrovent nasal spray) reduces the nasal response to Methacholine
J Allergy Clin Immunol 1992 Jun;89(6):1065-75.PMID:1535082DOI:10.1016/0091-6749(92)90290-i.
We investigated the efficacy of local ipratropium bromide on methacholine-induced nasal secretions in a double-blind, placebo-controlled experiment. Twenty subjects with perennial rhinitis received a total intranasal dose of 21, 42, 84, and 168 micrograms of ipratropium bromide or placebo in each nostril. One hour later, filter paper disks were used to deliver increasing doses of Methacholine and to collect secretions from the left septum. Concomitantly, symptoms of rhinorrhea and nasal congestion were scored. Compared with doses of placebo, all doses of ipratropium bromide significantly reduced the methacholine-induced increase in nasal secretion weights and symptoms of rhinorrhea (p less than 0.01). The highest dose was significantly more effective than the lower doses in reducing secretion weights (p = 0.01). We speculate that ipratropium bromide may prove beneficial for the treatment of rhinorrhea in perennial rhinitis. Furthermore, increasing the delivered dose to 168 micrograms may increase efficacy without augmenting side effects.
The effect of ipratropium bromide on nasal hypersecretion induced by Methacholine in patients with vasomotor rhinitis. A double-blind, cross-over, placebo-controlled and randomized dose-response study
Acta Otolaryngol 1988 Nov-Dec;106(5-6):453-9.PMID:2974675DOI:10.3109/00016488809122270.
The effect of various doses of ipratropium bromide aerosol on nasal hypersecretion induced by five concentrations Methacholine was studied in 24 patients with vasomotor rhinitis and excessive watery nasal secretion. The volume of nasal secretion was greater with each of the five increasing doses of Methacholine from 7.5 to 120 mg/ml. The median volume of nasal secretion was alike in all patients after administration of Methacholine only and after treatment by placebo followed by Methacholine. When the patients were treated with ipratropium bromide prior to administering Methacholine the volume of secretion was reduced significantly. With doses of 40 micrograms and 100 micrograms of ipratropium to each nostril a similar reduction in the volume of secretion occurred but a still greater reduction by the application of 200 micrograms of ipratropium when compared with treatment by the placebo. While the volume of secretion increased with each increasing concentration of Methacholine, a similar pattern of reduced secretion for each concentration of Methacholine was seen with each greater concentration of ipratropium. In patients with vasomotor rhinitis, treatment with ipratropium bromide was found to reduce significantly the hypersecretion induced by Methacholine when compared with treatment by the placebo. This reduction was greater with greater doses of ipratropium.
Prolonged effect of tiotropium bromide on methacholine-induced bronchoconstriction in asthma
Am J Respir Crit Care Med 1996 Oct;154(4 Pt 1):876-80.PMID:8887578DOI:10.1164/ajrccm.154.4.8887578.
Inhaled anticholinergic drugs are effective in the treatment of chronic obstructive pulmonary diseases (COPD), of acute asthma, and of some patients with nocturnal asthma. Tiotropium bromide (tiotropium) is a novel anticholinergic agent with a long duration of action and kinetic selectivity for M1- and M3-subtypes of muscarinic receptors. We investigated the duration of protection of a single dose of inhaled tiotropium against methacholine-induced bronchoconstriction in 12 male atopic asthmatic volunteers in a double-blind, placebo-controlled study. On four separate occasions 8 to 24 d apart, Methacholine PC20 was measured serially for up to 48 h after placebo and after three doses of tiotropium (10, 40, and 80 microg). Each dose of tiotropium produced mild bronchodilatation as measured by an increase in FEV1 of between 5.5 and 11.1% from baseline, that was sustained for 24 h. There was significant dose-dependent protection against Methacholine challenge at 2 h of 5.0 +/- 1.1, 7.1 +/- 0.5, and 7.9 +/- 0.7 (mean +/- SEM) doubling doses after 10, 40, and 80 microg respectively, and this persisted for 48 h. There were no adverse effects reported at any dose. The prolonged bronchodilator response and protection against Methacholine challenge suggest that tiotropium may be useful in the treatment of COPD and nocturnal asthma and that once-daily dosing may be sufficient.